GSK1059615

SKU: orb1223518

Description

GSK1059615 is a highly potent, dual PI3K/mTOR inhibitor with IC50 of 0.4 nM/0.6 nM/2 nM/5 nM and 12 nM for PI3Kα/β/δ/γ and mTOR, respectively; inhibits survival and proliferation of established (SCC-9, SQ20B and A253 lines) and primary human HNSCC cells, blocks PI3K-AKT-mTOR activation in HNSCC cells, induces programmed necrosis but not apoptosis, suppresses SCC-9 tumor growth in nude mice; strongly reduces neutrophil-sperm interaction with IC50 of <10 nM in cattle.Solid Tumors Phase 1 Discontinued(In Vitro):GSK1059615 inhibits PI3Kα, β, γ and δ, with Ki of 0.42 nM, 0.6 nM, 0.47 nM and 1.7 nM, respectively. In T47D and BT474 cancer cells, GSK1059615 inhibits the phosphorylation of Akt at S473, with IC50 of 40 nM.(In Vivo):GSK1059615 (25 mg/kg) effectively inhibits tumor growth in xenograft mice models of BT474 or HCC1954 breast cancer cells.

Key Properties

• CAS Number: 958852-01-2
• MW: 333.3638
• Purity: >98% (HPLC)
• Formula: C₁₈H₁₁N₃O₂S
• SMILES: c1cc2c(cc1/C=C\3/C(=O)NC(=O)S3)c(ccn2)c4ccncc4
• Target: PI3K
• Solubility: 10 mM in DMSO

Bioactivity

• In Vivo:
  GSK1059615 (25 mg/kg) effectively inhibits tumor growth in xenograft mice models of BT474 or HCC1954 breast cancer cells.
• In Vitro:
  GSK1059615 inhibits PI3Kα, β, γ and δ, with Ki of 0.42 nM, 0.6 nM, 0.47 nM and 1.7 nM, respectively. In T47D and BT474 cancer cells, GSK1059615 inhibits the phosphorylation of Akt at S473, with IC50 of 40 nM.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

GSK 1059615 | GSK-1059615

Quick Database Links

Gene Symbol

PI3K